Evidence map›Paper›PMID 40450579›Full record

ArticleJournal of medicinal chemistry2025

Optimization of Tambjamines Active against Multiple Stages of Malaria Parasites.

Amrendra Kumar, Yuexin Li, Xiaowei Zhang, Xiannu Jin, William E Dennis, Ravi Chetree, Cameron Blount, Diana Caridha, Michael S Madejczyk, Patricia J Lee and 30 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Journal of medicinal chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

3 citing papers in PubMed.

  1. Article
  2. Article
  3. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

40 authors.

Amrendra KumarDepartment of Chemistry, Portland State University, Portland, Oregon 97201, United States.
Yuexin LiDepartment of Veterans Affairs Medical Center, Portland, Oregon 97239, United States.
Xiaowei ZhangDepartment of Veterans Affairs Medical Center, Portland, Oregon 97239, United States.
Xiannu JinExperimental Therapeutics Branch, CIDR, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
William E DennisExperimental Therapeutics Branch, CIDR, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Ravi ChetreeExperimental Therapeutics Branch, CIDR, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Cameron BlountExperimental Therapeutics Branch, CIDR, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Diana CaridhaExperimental Therapeutics Branch, CIDR, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Michael S MadejczykExperimental Therapeutics Branch, CIDR, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Patricia J LeeExperimental Therapeutics Branch, CIDR, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Kristina PannoneExperimental Therapeutics Branch, CIDR, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Jesse DeLucaExperimental Therapeutics Branch, CIDR, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Chau VuongExperimental Therapeutics Branch, CIDR, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Susan LeedExperimental Therapeutics Branch, CIDR, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Hieu T DinhExperimental Therapeutics Branch, CIDR, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Kennedy MdakiExperimental Therapeutics Branch, CIDR, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Rohit MahatoTCG Lifesciences, Kolkata, West Bengal 700091, India.
Priyam SenTCG Lifesciences, Kolkata, West Bengal 700091, India.
Trisha MondalTCG Lifesciences, Kolkata, West Bengal 700091, India.
Karabi PhukanTCG Lifesciences, Kolkata, West Bengal 700091, India.
Ankur SahaTCG Lifesciences, Kolkata, West Bengal 700091, India.
Anongruk Chim-OngDepartment of Internal Medicine, Morsani College of Medicine, University of South Florida, Tampa, Florida 33612, United States.
Liwang CuiDepartment of Internal Medicine, Morsani College of Medicine, University of South Florida, Tampa, Florida 33612, United States.
Rajachandrasekhar ValmonDepartment of Chemistry, Portland State University, Portland, Oregon 97201, United States.
Sivanna ChithannaDepartment of Chemistry, Portland State University, Portland, Oregon 97201, United States.
Rozalia A DodeanDepartment of Chemistry, Portland State University, Portland, Oregon 97201, United States.ORCID 0000-0001-5002-4607
David H PeytonDepartment of Chemistry, Portland State University, Portland, Oregon 97201, United States.ORCID 0000-0001-5828-055X
Stephen OrenaInfectious Diseases Research Collaboration, Kampala, Uganda.
Jackson AssimweInfectious Diseases Research Collaboration, Kampala, Uganda.
Innocent TibagambirwaInfectious Diseases Research Collaboration, Kampala, Uganda.
Patrick AngutokoInfectious Diseases Research Collaboration, Kampala, Uganda.
Jennifer LegacDepartment of Medicine, University of California San Francisco, San Francisco, California 94143, United States.
Oriana KreutzfeldDepartment of Medicine, University of California San Francisco, San Francisco, California 94143, United States.
Philip J RosenthalDepartment of Medicine, University of California San Francisco, San Francisco, California 94143, United States.
Elodie ChenuMMV Medicines for Malaria Venture, Geneva CH-1215, Switzerland.
James DuffyMMV Medicines for Malaria Venture, Geneva CH-1215, Switzerland.
Alison RothExperimental Therapeutics Branch, CIDR, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Kevin A ReynoldsDepartment of Chemistry, Portland State University, Portland, Oregon 97201, United States.ORCID 0000-0003-0270-9809
Jane X KellyDepartment of Chemistry, Portland State University, Portland, Oregon 97201, United States.ORCID 0000-0001-8871-0207
Papireddy KancharlaDepartment of Chemistry, Portland State University, Portland, Oregon 97201, United States.ORCID 0000-0002-6381-1236

Funding

Resistance of Malaria Parasites to Artemisinin-Based TherapiesR01AI075045 · NIAID · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI ROSENTHAL, PHILIP JON · 2009 to 2024
$8.4M
Mechanisms of varied sensitivity of P. falciparum field isolates to the antimalarial drug pipelineR01AI139179 · NIAID · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI Philip Jon Rosenthal · 2018 to 2026
$6.3M
Novel Multiple-Stage Active AntimalarialsR01AI141972 · NIAID · PORTLAND STATE UNIVERSITY · PI JANE X KELLY, Papireddy Kancharla · 2019 to 2026
$4.5M
Unraveling the Drivers of Persistent Malaria Transmission in Cameroon: A Systems Approach (REDIAL)U19AI181593 · NIAID · UNIVERSITY OF SOUTH FLORIDA · PI LIWANG CUI · 2024 to 2026
$3.0M
Natural Product Inspired Novel Antimalarials with Radical Cure PotentialR01AI175444 · NIAID · PORTLAND STATE UNIVERSITY · PI JANE X KELLY, Papireddy Kancharla · 2023 to 2026
$2.5M
Resistance of Malaria Parasites to Artemisinin-Based Combination TherapiesR56AI075045 · NIAID · UNIVERSITY OF CALIFORNIA, SAN FRANCISCO · PI ROSENTHAL, PHILIP JON · 2008 to 2008
$618k
NIAID NIH HHS R01 AI075045NIAID NIH HHS R01 AI139179NIAID NIH HHS R01 AI141972NIAID NIH HHS R01 AI175444NIAID NIH HHS R56 AI075045NIAID NIH HHS U19 AI181593
6 · The paper itself

Abstract

Malaria remains a major global health challenge, demanding new therapies with novel mechanisms and multistage activity to overcome resistance. Previously, we developed a natural product-inspired novel antimalarial tambjamine chemotype that is potent against liver, asexual erythrocytic, and sexual erythrocytic parasite life cycle stages. Herein, we report a rigorous optimization strategy that expanded our chemical library and, more importantly, produced several lead tambjamines with excellent oral efficacy, while exhibiting feasible safety and metabolic profiles. Notably, KAR1123 (

Indexed as

AntimalarialsMalariaPlasmodium falciparumAnimalsDrug ResistanceFemaleHumansLife Cycle StagesMiceParasitic Sensitivity TestsPlasmodium bergheiPlasmodium yoeliiStructure-Activity RelationshipAntimalarials

Identifiers

PMID40450579
PMCPMC12163703

What OpenQuestion holds

Textmetadata
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Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.